NR566 Midterm
CYP3A4 Inhibition:
Increases levels of drugs like cisapride and warfarin (may
What are some important drug increase risk of side effects)
interactions to consider when
prescribing itraconazole? Drugs that raise gastric pH:
Can reduce itraconazole absorption (e.g., antacids, PPIs)
Itraconazole: Broad-spectrum azole antifungal
What is the primary function
Function: Treats systemic fungal infections
of itraconazole and how does
Advantages over Amphotericin B:Lower toxicityCan be
it compare to amphotericin
taken orally (oral administration)Alternative to Amphotericin
B?
B in many cases
Type: Narrow-spectrum echinocandin (IV)
What is the primary function Targets: Fungal cell wall
of caspofungin, and how does
it differ from other antifungal Effective against: Aspergillus and Candida
agents?
Comparison: Better tolerated than amphotericin B, similar efficacy
Invasive aspergillosis: For patients unresponsive to amphotericin B or
What are the key
itraconazole
therapeutic uses of
caspofungin? Systemic Candida infections: Including candidemia and intraabdominal
abscesses
-Treats superficial mycoses
What is the primary
-Specifically for dermatophytic infections of skin, hair, and nails
indication for
griseofulvin? (3) -Not effective against systemic mycoses or Candida species
, -Inhibits fungal mitosis by binding to microtubules
How does griseofulvin work to
-Deposited in keratin precursor cells
combat fungal infections?
(3) -Newly formed keratin becomes resistant to fungal invasion
-Treats onychomycosis (fungal nail infections)
What are the primary
indications for oral
-Effective for dermatophyte infections (e.g., ringworm)
terbinafine? (2)
-Inhibits squalene epoxidase
What is the mechanism of
-Reduces ergosterol synthesis
action of terbinafine? (3)
-Highly active against dermatophytes; less effective against Candida
-Higher risk for achlorhydria (condition in which the stomach
produces little or no hydrochloric acid) affecting
What considerations should be
absorption
taken when prescribing
azoles like itraconazole to
-Increased plasma levels of medications (e.g., warfarin, phenytoin)
older adults? (3)
-Need for careful medication reconciliation due to polypharmacy
-Age-related changes in metabolism and excretion
What factors affect the
-Ability to self-administer medications safely
pharmacokinetics of azoles
in older adults? (3) -Risk of drug interactions with multiple medications
Poorly absorbed from the GI tract; requires IV
administration Extensive binding to sterol-
What the key pharmacokinetic
properties of amphotericin
containing membranes
B? (4)
Limited penetration to cerebrospinal fluid (CSF)
Long elimination time; detectable in tissues for over a year
High incidence of infusion reactions
(fever, chills) Nephrotoxicity is common;
What are the major
considerations regarding
renal function should be monitored Use with
amphotericin B's toxicity? (4)
caution in patients taking other
, nephrotoxic drugs
Should only be used for life-threatening infections due to toxicity
What is the treatment of choice amphotericin B
for most systemic mycoses?
What are the alternatives to Azoles (e.g., itraconazole, fluconazole, voriconazole) serve as
amphotericin B for systemic alternatives.
mycoses and what are their
Advantages: Lower toxicity and can be given orally.
advantages?
What is the main drug inhibits CYPA4 increasing levels of drugs like: cisapride,
interaction concern with pimozide, dofetilide, quinidine (risk of ventricular
itraconazole? dysrhythmias)
Antacids, H2 antagonists, and proton pump inhibitors can
How do drug that raise gastric reduce absorption of itraconazole.
pH affect itraconazle? (2)
These agents should be given at least 1 hour before or 2 hours after
itraconazole.
CYP3A4 Inhibition:
Increases levels of drugs like cisapride and warfarin (may
What are some important drug increase risk of side effects)
interactions to consider when
prescribing itraconazole? Drugs that raise gastric pH:
Can reduce itraconazole absorption (e.g., antacids, PPIs)
Itraconazole: Broad-spectrum azole antifungal
What is the primary function
Function: Treats systemic fungal infections
of itraconazole and how does
Advantages over Amphotericin B:Lower toxicityCan be
it compare to amphotericin
taken orally (oral administration)Alternative to Amphotericin
B?
B in many cases
Type: Narrow-spectrum echinocandin (IV)
What is the primary function Targets: Fungal cell wall
of caspofungin, and how does
it differ from other antifungal Effective against: Aspergillus and Candida
agents?
Comparison: Better tolerated than amphotericin B, similar efficacy
Invasive aspergillosis: For patients unresponsive to amphotericin B or
What are the key
itraconazole
therapeutic uses of
caspofungin? Systemic Candida infections: Including candidemia and intraabdominal
abscesses
-Treats superficial mycoses
What is the primary
-Specifically for dermatophytic infections of skin, hair, and nails
indication for
griseofulvin? (3) -Not effective against systemic mycoses or Candida species
, -Inhibits fungal mitosis by binding to microtubules
How does griseofulvin work to
-Deposited in keratin precursor cells
combat fungal infections?
(3) -Newly formed keratin becomes resistant to fungal invasion
-Treats onychomycosis (fungal nail infections)
What are the primary
indications for oral
-Effective for dermatophyte infections (e.g., ringworm)
terbinafine? (2)
-Inhibits squalene epoxidase
What is the mechanism of
-Reduces ergosterol synthesis
action of terbinafine? (3)
-Highly active against dermatophytes; less effective against Candida
-Higher risk for achlorhydria (condition in which the stomach
produces little or no hydrochloric acid) affecting
What considerations should be
absorption
taken when prescribing
azoles like itraconazole to
-Increased plasma levels of medications (e.g., warfarin, phenytoin)
older adults? (3)
-Need for careful medication reconciliation due to polypharmacy
-Age-related changes in metabolism and excretion
What factors affect the
-Ability to self-administer medications safely
pharmacokinetics of azoles
in older adults? (3) -Risk of drug interactions with multiple medications
Poorly absorbed from the GI tract; requires IV
administration Extensive binding to sterol-
What the key pharmacokinetic
properties of amphotericin
containing membranes
B? (4)
Limited penetration to cerebrospinal fluid (CSF)
Long elimination time; detectable in tissues for over a year
High incidence of infusion reactions
(fever, chills) Nephrotoxicity is common;
What are the major
considerations regarding
renal function should be monitored Use with
amphotericin B's toxicity? (4)
caution in patients taking other
, nephrotoxic drugs
Should only be used for life-threatening infections due to toxicity
What is the treatment of choice amphotericin B
for most systemic mycoses?
What are the alternatives to Azoles (e.g., itraconazole, fluconazole, voriconazole) serve as
amphotericin B for systemic alternatives.
mycoses and what are their
Advantages: Lower toxicity and can be given orally.
advantages?
What is the main drug inhibits CYPA4 increasing levels of drugs like: cisapride,
interaction concern with pimozide, dofetilide, quinidine (risk of ventricular
itraconazole? dysrhythmias)
Antacids, H2 antagonists, and proton pump inhibitors can
How do drug that raise gastric reduce absorption of itraconazole.
pH affect itraconazle? (2)
These agents should be given at least 1 hour before or 2 hours after
itraconazole.
